Pharmaceutical Composition for the Treatment of Solar Urticaria

a technology for solar urticaria and pharmaceutical compositions, applied in the field of local anesthesia, can solve the problems of inability to establish a hypothesis, poorly understood pathogenesis of solar urticaria, and largely unknown how and why mast cells are activated in patients, and achieve the effect of low side effects and convenient patient treatmen

Inactive Publication Date: 2011-12-01
CHARITE UNIVS MEDIZIN BERLIN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0045]The effectiveness of EMLA® suggests that an application of the active compounds comprised in EMLA® prior to UV-provocation stabilizes or inhibits sensory nerve fibres of the skin and induces down-regulation or inhibition of the release of pro-inflammatory neuropeptides. Due to this more general concept it is assumed that (1) other local anesthetics in addition to lidocaine and prilocaine, (2) lidocaine alone or prilocaine alone, and (3) lidocaine and / or prilocaine in combination with other local anesthetics are effective as well

Problems solved by technology

However, it is largely unknown how and why mast cells are activated in patients with physical urticaria, i.e. what signals are responsible for mast cell activation and what causes them to come about.
The pathogenesis of solar urticaria, however, is still poorly understood.
Yet, the hypothesis is not established.
Nonsedating H1-antihistamines are the first line therapy for solar urticaria, but in severe cases conventional antihistaminic treatment is often unsuccessful.
High-grade sun blockers are usually not sufficient, and light-hardening therapy, although sometimes quite effective, is not appropriate for long-term treatment because of the risk of skin tumour development.
However, omalizumab is currently not licensed for urticaria, is very expensive, and data from clinical trials with larger patient numbers are missing.

Method used

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  • Pharmaceutical Composition for the Treatment of Solar Urticaria
  • Pharmaceutical Composition for the Treatment of Solar Urticaria
  • Pharmaceutical Composition for the Treatment of Solar Urticaria

Examples

Experimental program
Comparison scheme
Effect test

example 1

1.1. Subjects

[0054]Subjects to this experiment were two solar urticaria patients, one male (aged 29) and one female (aged 36). Both patients were sensitive to UVA-radiation (FIG. 1).

1.2. Pharmaceutical Preparation

[0055]EMLA® is a topical anaesthetic cream (a eutectic mixture of lidocaine and prilocaine) widely used for superficial anaesthesia of the skin before taking blood samples or prior to superficial skin surgery. 1 g of EMLA® cream (Astra Zeneca) contains 25 mg lidocaine (i.e. 2.5% by weight) and 25 mg prilocaine (i.e. 2.5% by weight).

1.3. Experimental Protocol

[0056]The patients with solar urticaria and action spectrum to UVA underwent skin microdialysis after UVA provocation.

[0057]Microdialysis is a well-established technique for the continuous sampling of small, water-soluble molecules within the extracellular fluid space in vivo. It has the advantage over other sampling techniques in that it can be used in intact tissues to follow temporal variations in the generation and t...

example 2

[0062]For comparison study, UV-provocation (and microdialysis) was performed a second time in skin without previous sun exposure, namely the buttocks. Thus, the female patient of Example 1 underwent the same procedure as described in Example 1 for the volar forearm again on the buttocks. A control area was irradiated with UVA but without prior application of EMLA® (FIG. 4).

[0063]Fifteen min after UVA radiation an erythema developed in both skin sites previously treated with and without EMLA®. A whealing reaction was seen after 15 min in the non-EMLA® skin site and after 20 min in the EMLA®-treated skin area, but less pronounced. After 30 min the clinical symptoms (wheal and erythema size) were much more pronounced in the non-EMLA® skin site compared to the anaesthesized site (FIG. 5). The kinetics of skin lesion development after 30 min was also documented by digital time lapse photography (FIG. 6).

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Abstract

The present invention refers to a local anesthetic, preferably selected from the group of aminoamide local anesthetics, in particular lidocaine or prilocaine, for use in the treatment or prevention of physical urticaria, in particular solar urticaria. The present invention further refers to a pharmaceutical composition, e.g. a cream, comprising such a local anesthetic, in particular a combination of lidocaine and prilocaine.

Description

CROSS-REFERENCE TO A RELATED APPLICATION[0001]This application claims priority to European Patent Application No. 10003676.3, filed Apr. 1, 2010, which is incorporated herein by reference in its entirety.FIELD OF INVENTION[0002]The present invention refers to local anesthetics, in particular lidocaine and / or prilocaine, in the treatment or prevention of physical urticaria, in particular solar urticaria.BACKGROUND OF THE INVENTION[0003]Physical urticarias are characterized by wheal-and-flare-type skin reactions and / or angioedema following exposure to a specific, exogenous, physical stimulus. The different subtypes are classified according to their eliciting physical trigger. These include thermal triggers (cold or heat contact), electromagnetic radiation (usually UVA or visible light), and mechanical triggers (friction, pressure, or vibration) (Zuberbier et al., 2006).[0004]The symptoms of physical urticarias are caused by the activation of skin mast cells and subsequent release of h...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/167A61P17/00
CPCA61K9/0014A61K31/167A61K2300/00A61P17/00A61P17/02
Inventor MAURER, MARCUSMETZ, MARTINKRAUSE, KAROLINE
Owner CHARITE UNIVS MEDIZIN BERLIN
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